Corticosteroids Flashcards
What drug/ hormone is a mineralocorticoid?
Aldosterone
What drug/ hormone is a glucocorticoid?
Cortisol
What is aldosterone regulated by?
ATII and K+
What is cortisol regulated by?
ACTH
What are the 2 main effects of aldosterone?
↑ Na+ and H2O retention and ↑ K+ excretion
What does cortisol exert a negative feedback effect on?
CRH = ↓ ACTH
Is cortisol a short or long acting stress hormone?
Long acting (acts via nuclear receptors)
Does cortisol favor catabolic or anabolic processes?
Catabolic (favors energy release) (↑ circulating glucose, FFA, AA)
Cortisol antagonizes the effects of what hormone?
Insulin
How does cortisol play a role in fat redistribution?
Redistribution of fat centrally
What are the CV effects of cortisol (2)
↑ vascular responsiveness to sympathetic stimulation b/c inhibition of catecholamine re-uptake (more catecholamines in cleft = more effects), ↑ CO
Cortisol has endocrine effects by decreasing what hormones?
GH, TSH, LH
Cortisol has endocrine effects by increasing what hormone?
Epi
How does cortisol lead to bone destruction over time? (2)
Inhibits action of vit. D → ↓ Ca deposition ↑ PTH → ↑ Ca loss from bone
What are the effects of cortisol on the immune system?
Immunosuppressive, anti-inflammatory, suppression of wound healing (early and late stages)
What effects can cortisol have on the CNS, although there is individual variance? (5)
Mood elevation, insomnia/ restlessness, anxiety, depression, psychosis
What is the possible GI related SE of cortisol?
Peptic ulcer development
Is Cushing’s glucocorticoid excess or insufficiency?
Excess
What is the cause of Cushing’s disease?
Excess ACTH due to tumor in the pituitary gland
What is the cause of Cushing’s syndrome?
Excess cortisol due to anything else besides ACTH secreting pituitary tumor
What is the most common cause of Cushing’s syndrome?
Exogenous glucocorticoids (could also be a tumor)
What are the following sxs associated with?
Buffalo hump, thinning of skin, thin arms, moon face, increased abdominal fat, striae, easy bruising, poor wound healing
Cushing’s
What test is performed for the diagnosis of Cushing’s after a low dose dexamethasone suppression test?
High dose dexamethasone suppression test
For the high dose dexamethasone suppression test, you measure baseline cortisol levels in AM, administer dexamethasone in the PM, then measure levels again when?
The following morning (when it should be the highest due to circadian release)
On the high dose dexamethasone suppression test, extreme suppression of cortisol indicates what?
Normal
On the high dose dexamethasone suppression test, cortisol levels 50% suppressed indicate what?
Cushing’s disease
On the high dose dexamethasone suppression test, unchanged cortisol levels indicate what?
Cushing’s syndrome
Addison’s disease, adrenal malfunction, and pituitary malfunction lead to adrenocortical excess or insufficiency?
Insufficiency
What are the sxs of adrenocortical insufficiency? (4)
Hyperpigmentation, salt craving, anorexia, weight loss
Acute adrenal insufficiency is aka?
Addisonian crisis
Circulatory collapse, dehydration, vomiting, hyperkalemia, and the possibility of these sxs to be fatal is what condition?
Addisonian crisis
Condition in which the body is unable to repond to acute high stress so need exogenous mineralocorticoid to appropriately respond to stress is what?
Addisonian crisis
Ketoconazole drug class?
Corticosteroid synthesis inhibitor
Mifipristone drug class? (corticosteroids)
Receptor antagonists
Spironolactone drug class (corticosteroids)
Receptor antagonists
What is the relative mineralocorticoid (salt-retaining) and glucocorticoid (anti-inflammatory) activity of hydrocortisone and cortisone?
Equal activity
What is the relative mineralocorticoid (salt-retaining) and glucocorticoid (anti-inflammatory) activity of prednisone and prednisolone?
Glucocorticoid > mineralocorticoid
What is the relative mineralocorticoid (salt-retaining) and glucocorticoid (anti-inflammatory) activity of methylprednisolone and triamcinolone?
Virtually no mineralocorticoid activity
Is hydrocortisone or cortisone inactive?
Cortisone inactive, 80% potency
Is prednisone or prednisolone inactive?
Prednisone
What is the primary use of hydrocortisone and cortisone?
Replacement therapy for adrenal insufficiency
What is the duration of hydrocortisone and cortisone?
Short duration (8-12 hours)
What is the primary use of prednisone and prednisolone?
Anti-inflammatory effects (with minor salt-retaining effects)
What is the duration of prednisone and prednisolone?
Intermediate duration (12-36 hours)
What is the use of methylprednisone and triamcinolone?
Anti-inflammatory (with no salt-retaining effects)
What is the duration of methylprednisone and triamcinolone?
Intermediate duration (12-36 hours)
What is the use of dexamethasone and betamethasone?
Anti-inflammatory (with no salt-retaining effects)
What is the duration of dexamethasone and betamethasone?
Long duration (36-72 hours)
What is the use of fluticasone?
Most commonly prescribed inhaled mineralocorticoid
What is the use of aldosterone?
Salt-retaining with minimal anti-inflammatory effects
What is the use of fludrocortisone?
Salt retaining with minimal anti-inflammatory effects
What is the use of oral corticosteroids?
High dose/ long-term therapy or replacement therapy
What is the use of corticosteroid injections?
Emergencies or depot administration
What is the use of inhalation/ intranasal corticosteroids?
Asthma and rhinitis
What are the 3 notable properties/ effects of topical corticosteroids?
Insoluble (prevents absorption), more potent used on thick skin only (if skin damage/ thin skin → systemic absorption), repeated application = depot effect
What is the danger about acute adrenal insufficiency?
Can be life threatening
When will you see increased amounts of corticosteroids?
Stress or infection
What is the DOC for initial treatment of asthma?
Inhaled glucocorticoid
Why are corticosteroids used in the treatment of RA?
Decrease inflammation
(used in inflammatory conditions in general)
What therapeutic guideline should be followed for corticosteroid treatment with respect for amount of time and dose given?
Only as long as necessary at lowest effective dose
Should you start corticosteroid treatment at a high or low dose?
Start at higher dose, taper down once inflammation is under control
Should corticosteroids be used locally or diffuse?
Locally whenever possible
Should corticosteroids be given daily or an alternate days?
Alternate days
When are corticosteroids most likely to cause adverse effects and result in suppressed HPA (for months)?
Chronic or high dose
(short term therapy (1-2 weeks) is not likely to cause serious problems)
What is the worst adverse effect of corticosteroid treatment that limits therapeutic effects?
Osteoporosis
How does corticosteroid treatment affect infection?
Masks sxs of infection/ makes more susceptible to infection (this can lead to serious infection)
How can corticosteroid treatment after diabetes pts?
Hyperglycemia (may “unmask” DM in some pts)
What are some of the adverse CNS effects seen with corticosteroid treatment? (seen with acute or chronic txs)
Restlessness, insomnia, psychosis, increased appetite
Why should you avoid abrupt cessation or more than 1-2 weeks of high dose therapy with corticosteroids? (2)
Induce adrenal insufficiency/ HPA depression
Can cause cushingoid SEs
How can corticosteroid treatment affect chronic pts?
Stress intolerance
When are there no contraindications to corticosteroid treatment?
Adrenal insufficiency
The following are contraindications to what?
Systemic bacterial or viral infection, poorly controlled DM, osteoporosis, heart disease or HTN w/ CHF, IMC, pregnancy, childhood
Corticosteroid treatment with NO adrenal insufficiency
What is the MOA of ketoconazole besides antifungal?
Inhibits steroidogenesis (cortisol) production at high doses
What is the DOC in pre-surgical Cushing’s pts?
Ketoconazole
What are the SEs of ketoconazole? (4)
Reversible hepatotoxicity, gynecomastia, libido decrease, impotence
What is the contraindication to ketoconazole?
Pregnancy
What are the basic MOAs for spironolactone besdies potassium sparing diuretic? (as corticosteroid)
Mineralocorticoid, anti-androgen
What are the uses for spironolactone (corticosteroids)? (2)
Hyperaldosteronism, hisutism
